Date published: 2026-4-24

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Aldose Reductase Inhibitors

Aldose reductase is an enzyme predominantly involved in the polyol pathway, playing a critical role in the conversion of glucose to sorbitol. This enzyme's activity is pivotal in cellular processes, particularly under conditions of hyperglycemia where glucose availability exceeds metabolic demand, leading to an increased flux through the polyol pathway. Aldose reductase facilitates the first step in this pathway, reducing aldose sugars to their corresponding alcohol form, utilizing NADPH as a reducing agent. This biochemical reaction is essential for the osmoregulation of cells, as the accumulation of sorbitol can affect cellular osmolarity and contribute to various cellular dysfunctions. The enzyme is ubiquitously expressed in many tissues, including the lens of the eye, nerves, kidneys, and blood vessels, where its activity is linked to the metabolic management of glucose and the mitigation of osmotic stress induced by hyperglycemia. The inhibition of aldose reductase has been extensively studied, focusing on the interruption of the polyol pathway to prevent or mitigate the adverse effects of excess intracellular sorbitol. Inhibition strategies are centered on blocking the enzyme's active site, preventing the binding of its aldose sugar substrates. This can be achieved through the design of molecules that mimic the structure of the enzyme's natural substrates or products, thus competitively inhibiting the enzyme by occupying its active site. Non-competitive inhibitors have also been explored, which bind to sites other than the active site, inducing conformational changes that reduce the enzyme's affinity for its substrates. These inhibition mechanisms are crucial for understanding the enzyme's role in cellular physiology and for exploring the biochemical pathways involved in the management of intracellular glucose levels. The study of aldose reductase and its inhibition encompasses a significant area of biochemical research, focusing on elucidating the enzyme's structure-function relationship, the dynamics of its interaction with inhibitors, and its impact on cellular homeostasis under conditions of altered glucose metabolism.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Epalrestat

82159-09-9sc-218319
10 mg
$200.00
2
(1)

Epalrestat is another Aldose Reductase inhibitor used in the treatment of diabetic neuropathy. It works by reducing the conversion of glucose to sorbitol.

Alrestatin

51411-04-2sc-201443
sc-201443A
10 mg
50 mg
$113.00
$510.00
(0)

Alrestatin is an Aldose Reductase inhibitor that has been used in research to study the role of Aldose Reductase in diabetic cataracts.

Statil

72702-95-5sc-361367
100 mg
$235.00
1
(1)

Ponalrestat is a potent Aldose Reductase inhibitor that has been evaluated for its therapeutic potential in diabetic neuropathy.

2-Chloro-1-(4-fluorobenzyl)benzimidazole

84946-20-3sc-206422
1 g
$130.00
(0)

2-Chloro-1-(4-fluorobenzyl)benzimidazole exhibits notable interactions with aldose reductase, primarily through its halogen substituents, which enhance binding affinity. The compound's unique electronic properties facilitate the modulation of enzyme kinetics, potentially altering substrate accessibility. Its rigid benzimidazole framework promotes effective stacking interactions with aromatic residues in the active site, influencing catalytic efficiency. This compound's distinct structural features may also impact conformational dynamics, affecting enzyme regulation.

EBPC

57056-57-2sc-203572
sc-203572A
10 mg
50 mg
$115.00
$485.00
(0)

EBPC demonstrates a unique ability to interact with aldose reductase through its specific functional groups, which create a favorable environment for enzyme-substrate binding. The compound's steric configuration allows for optimal orientation within the active site, enhancing catalytic turnover rates. Additionally, its electron-withdrawing characteristics can influence the enzyme's redox state, potentially altering reaction pathways. The presence of multiple substituents contributes to its distinct conformational flexibility, impacting overall enzyme activity.

TCS PIM-1 4a

438190-29-5sc-296450
sc-296450A
10 mg
50 mg
$64.00
$346.00
(0)

TCS PIM-1 4a exhibits remarkable specificity for aldose reductase, facilitated by its unique structural motifs that stabilize enzyme interactions. Its rigid framework promotes effective substrate alignment, enhancing binding affinity. The compound's ability to modulate the enzyme's conformational dynamics can lead to altered kinetic profiles, influencing reaction rates. Furthermore, its unique electronic properties may affect the enzyme's catalytic mechanism, providing insights into substrate channeling and product formation.

Tolrestat

82964-04-3sc-474725
10 mg
$250.00
(0)

Tolrestat is another Aldose Reductase inhibitor that has been tested for its effects on diabetic complications.

Benfotiamine

22457-89-2sc-204639
sc-204639A
250 mg
1 g
$52.00
$171.00
(0)

While not a direct Aldose Reductase inhibitor, benfotiamine is a synthetic derivative of thiamine (vitamin B1) that can inhibit the activation of the enzyme and prevent the accumulation of sorbitol.